公开(公告)号：EP0752873A1

公开(公告)日：1997-01-15

申请号：EP95911829.0

申请日：1995-02-21

申请人： MALLINCKRODT MEDICAL, INC.

发明人： MERTENS, John ,  TOURWE, Dirk ,  CEUSTERS, Marc

IPC分类号： A61K51 ,  A61K31 ,  A61K38 ,  A61K49 ,  A61P35 ,  C07K1 ,  C07K5 ,  C07K7 ,  C07K17

CPC分类号： A61K51/08 ,  A61K38/00 ,  A61K51/085 ,  A61K51/088 ,  A61K2121/00 ,  A61K2123/00 ,  C07K7/083

摘要： The invention relates to a labelled peptide compound, wherein the peptide has a selective neurotensin receptor affinity and is represented by the general formula (I): R1 - (1Pro)n - ?2Xaa - 3Xbb -4Xcc - 5Xdd - 6Xee - 7¿Leu - OH, wherein R¿1? is a (C1-C3)alkanoyl group, an arylcarbonyl group, an aryl-(C1-C3)alkanoyl group, or a chelating group attached by an amide bond or through a spacing group to the peptide molecule; Xaa and Xbb are each individually Arg or Lys; Xcc is an unsubstituted or substituted cyclic amino acid, preferably selected from Pro and Hyp; Xdd is Tyr, Trp or Phe; Xee is Leu, Ile or t.-butylalanine; and n is 0 or 1; and wherein said peptide is labelled with (a) a metal isotope, or (b) with a radioactive halogen isotope; on the understanding that: (i) if the label is a metal isotope, R1 represents a chelating group for chelating said isotope; and (ii) if the label is a radioactive halogen isotope, said halogen isotope is attached to ?4¿Tyr in the 2-position of the phenyl ring, to 4Trp, or to the aryl group of substituent R¿1?. The invention further relates to a pharmaceutical composition comprising said labelled peptide compound, to the use of said composition for diagnosis and therapy, and to a kit for preparing a radiopharmaceutical composition.